RU2593756C2 - Конденсированные производные аминодигидротиазина, пригодные в качестве ингибиторов васе - Google Patents
Конденсированные производные аминодигидротиазина, пригодные в качестве ингибиторов васе Download PDFInfo
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- RU2593756C2 RU2593756C2 RU2013138717/04A RU2013138717A RU2593756C2 RU 2593756 C2 RU2593756 C2 RU 2593756C2 RU 2013138717/04 A RU2013138717/04 A RU 2013138717/04A RU 2013138717 A RU2013138717 A RU 2013138717A RU 2593756 C2 RU2593756 C2 RU 2593756C2
- Authority
- RU
- Russia
- Prior art keywords
- trifluoromethyl
- compound
- furo
- amino
- tetrahydro
- Prior art date
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- YJOUUQFWUULCQB-RNRVQEDPSA-N CCOc(nc1)cnc1C(Nc(cc1)cc([C@@]23N=C(N)SC[C@@H]2[C@@H](C(F)(F)F)OC3)c1F)=O Chemical compound CCOc(nc1)cnc1C(Nc(cc1)cc([C@@]23N=C(N)SC[C@@H]2[C@@H](C(F)(F)F)OC3)c1F)=O YJOUUQFWUULCQB-RNRVQEDPSA-N 0.000 description 2
- MWUCVUDHOLYUAM-UHFFFAOYSA-N CC(C)(C)OC(COC(C(F)(F)F)C=C)=O Chemical compound CC(C)(C)OC(COC(C(F)(F)F)C=C)=O MWUCVUDHOLYUAM-UHFFFAOYSA-N 0.000 description 1
- XVZHCMCNUQXSDN-UXWZTASCSA-N CC(C1)([C@@]23N=C(N)SC[C@@H]2[C@@H](C(F)(F)F)OC3)C(F)=CC=C1NC(c(cc1)ncc1OC)=O Chemical compound CC(C1)([C@@]23N=C(N)SC[C@@H]2[C@@H](C(F)(F)F)OC3)C(F)=CC=C1NC(c(cc1)ncc1OC)=O XVZHCMCNUQXSDN-UXWZTASCSA-N 0.000 description 1
- 0 CC1C(C23*=C(*)NCC2(C)[C@@](NC=C)OC3)=CC(*(C(C2=C*C(*)=C*2)O)=C)=CC1* Chemical compound CC1C(C23*=C(*)NCC2(C)[C@@](NC=C)OC3)=CC(*(C(C2=C*C(*)=C*2)O)=C)=CC1* 0.000 description 1
- OKIAKMUNNXFYCX-DJCROIMJSA-N Cc(nc1)cnc1C(Nc(cc1F)cc([C@@]23N=C(N)SC[C@@H]2[C@@H](C(F)(F)F)OC3)c1F)=O Chemical compound Cc(nc1)cnc1C(Nc(cc1F)cc([C@@]23N=C(N)SC[C@@H]2[C@@H](C(F)(F)F)OC3)c1F)=O OKIAKMUNNXFYCX-DJCROIMJSA-N 0.000 description 1
- QNUMYBQXKOPVDO-JZQLECPJSA-N FC([C@H]1OCC2(c(cccc3)c3F)NOCC12)(F)F Chemical compound FC([C@H]1OCC2(c(cccc3)c3F)NOCC12)(F)F QNUMYBQXKOPVDO-JZQLECPJSA-N 0.000 description 1
- SZTOKSLPOMRAMF-HNJNHCNJSA-N NC(SC[C@@H]1[C@@H](C(F)(F)F)OC2)=N[C@]12c(cc(cc1)NC(c2ncc(C(F)(F)F)cc2)=O)c1F Chemical compound NC(SC[C@@H]1[C@@H](C(F)(F)F)OC2)=N[C@]12c(cc(cc1)NC(c2ncc(C(F)(F)F)cc2)=O)c1F SZTOKSLPOMRAMF-HNJNHCNJSA-N 0.000 description 1
- OISNOLXGBCPNDK-OVWKYPIYSA-N NC(SC[C@@H]1[C@@H](C(F)(F)F)OC2)=N[C@]12c(cc(cc1)NC(c2ncc(C(F)(F)F)nc2)=O)c1F Chemical compound NC(SC[C@@H]1[C@@H](C(F)(F)F)OC2)=N[C@]12c(cc(cc1)NC(c2ncc(C(F)(F)F)nc2)=O)c1F OISNOLXGBCPNDK-OVWKYPIYSA-N 0.000 description 1
- KEAXHJHDEOLCCG-UHFFFAOYSA-N NC1(C(CO)C(C(F)(F)F)OC1)c(cccc1)c1F Chemical compound NC1(C(CO)C(C(F)(F)F)OC1)c(cccc1)c1F KEAXHJHDEOLCCG-UHFFFAOYSA-N 0.000 description 1
Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB1101140.0 | 2011-01-21 | ||
GBGB1101140.0A GB201101140D0 (en) | 2011-01-21 | 2011-01-21 | Fused aminodihydrothiazine derivatives |
PCT/EP2012/050833 WO2012098213A1 (en) | 2011-01-21 | 2012-01-20 | Fused aminodihydrothiazine derivatives useful as bace inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
RU2013138717A RU2013138717A (ru) | 2015-02-27 |
RU2593756C2 true RU2593756C2 (ru) | 2016-08-10 |
Family
ID=43769479
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2013138717/04A RU2593756C2 (ru) | 2011-01-21 | 2012-01-20 | Конденсированные производные аминодигидротиазина, пригодные в качестве ингибиторов васе |
Country Status (21)
Country | Link |
---|---|
US (3) | US8338407B2 (uk) |
EP (1) | EP2665732B1 (uk) |
JP (1) | JP5947815B2 (uk) |
KR (1) | KR101906466B1 (uk) |
CN (1) | CN103328486B (uk) |
AR (1) | AR084903A1 (uk) |
AU (1) | AU2012208526B2 (uk) |
BR (1) | BR112013018602A2 (uk) |
CA (1) | CA2828738A1 (uk) |
CL (1) | CL2013002083A1 (uk) |
ES (1) | ES2575914T3 (uk) |
GB (1) | GB201101140D0 (uk) |
IL (1) | IL226596A (uk) |
MX (1) | MX2013007917A (uk) |
PE (1) | PE20141182A1 (uk) |
RU (1) | RU2593756C2 (uk) |
SG (1) | SG190908A1 (uk) |
TW (1) | TW201309710A (uk) |
UA (1) | UA109927C2 (uk) |
WO (1) | WO2012098213A1 (uk) |
ZA (1) | ZA201303801B (uk) |
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CN103936690B (zh) | 2005-10-25 | 2016-06-08 | 盐野义制药株式会社 | 氨基二氢噻嗪衍生物 |
EP2147914B1 (en) | 2007-04-24 | 2014-06-04 | Shionogi&Co., Ltd. | Aminodihydrothiazine derivatives substituted with cyclic groups |
JP5383483B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | アルツハイマー症治療用医薬組成物 |
RU2476431C2 (ru) | 2008-01-18 | 2013-02-27 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Конденсированное производное аминодигидротиазина |
ES2738123T3 (es) | 2008-06-13 | 2020-01-20 | Shionogi & Co | Derivado heterocíclico que contiene azufre que tiene actividad inhibitoria de ß-secretasa |
JPWO2010047372A1 (ja) | 2008-10-22 | 2012-03-22 | 塩野義製薬株式会社 | Bace1阻害活性を有する2−アミノピリミジン−4−オンおよび2−アミノピリジン誘導体 |
GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
US8569310B2 (en) | 2009-10-08 | 2013-10-29 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use |
EP2485591B1 (en) | 2009-10-08 | 2016-03-23 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
BR112012013854A2 (pt) | 2009-12-11 | 2019-09-24 | Shionogi & Co | derivados de oxazina. |
JP5766198B2 (ja) | 2010-10-29 | 2015-08-19 | 塩野義製薬株式会社 | 縮合アミノジヒドロピリミジン誘導体 |
US8927721B2 (en) | 2010-10-29 | 2015-01-06 | Shionogi & Co., Ltd. | Naphthyridine derivative |
GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
GB201101139D0 (en) * | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
ES2624288T3 (es) | 2011-01-21 | 2017-07-13 | Eisai R&D Management Co., Ltd. | Métodos y compuestos útiles en la síntesis de derivados de aminodihidrotiazina condensados |
US8883779B2 (en) | 2011-04-26 | 2014-11-11 | Shinogi & Co., Ltd. | Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them |
EP2763676B1 (en) * | 2011-10-03 | 2019-12-25 | The University of Utah Research Foundation | Application of 5-ht6 receptor antagonists for the alleviation of cognitive deficits of down syndrome |
WO2014015125A1 (en) | 2012-07-19 | 2014-01-23 | Eisai R&D Management Co., Ltd. | Fused aminodihydrothiazine derivative salts and uses thereof |
GB201212816D0 (en) * | 2012-07-19 | 2012-09-05 | Eisai Ltd | Novel compounds |
US9618522B2 (en) * | 2012-09-05 | 2017-04-11 | Emory University | Diagnostic testing in dementia and methods related thereto |
WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
TWI593692B (zh) | 2013-03-12 | 2017-08-01 | 美國禮來大藥廠 | 四氫吡咯并噻嗪化合物 |
JO3318B1 (ar) | 2013-06-18 | 2019-03-13 | Lilly Co Eli | مثبطات bace |
TWI599358B (zh) * | 2014-09-16 | 2017-09-21 | 美國禮來大藥廠 | 組合療法 |
AR103680A1 (es) | 2015-02-23 | 2017-05-24 | Lilly Co Eli | Inhibidores selectivos de bace1 |
WO2016149057A1 (en) * | 2015-03-19 | 2016-09-22 | Eli Lilly And Company | Selective bace1 inhibitors |
AR104241A1 (es) * | 2015-04-29 | 2017-07-05 | Lilly Co Eli | Derivados de tetrahidrofuro tiazina como inhibidores de bace1 selectivos |
AR107774A1 (es) * | 2016-03-16 | 2018-05-30 | Lilly Co Eli | Terapia de combinación, método para el tratamiento de la enfermedad de alzheimer |
KR20170108203A (ko) * | 2016-03-16 | 2017-09-27 | 주식회사 피플바이오 | 응집형-형성 폴리펩타이드의 응집형을 검출하는 방법 |
TWI675034B (zh) * | 2016-05-20 | 2019-10-21 | 美商美國禮來大藥廠 | 四氫呋喃并<img align="absmiddle" height="18px" width="27px" file="d10999.TIF" alt="其他非圖式 ed10999.png" img-content="tif" orientation="portrait" inline="yes" giffile="ed10999.png"></img>化合物及其作為選擇性BACE1抑制劑之用途 |
US20190365774A1 (en) * | 2016-08-18 | 2019-12-05 | Eli Lilly And Company | Combination therapy of bace-1 inhibitor and anti-n3pglu abeta antibody |
TWI669119B (zh) * | 2016-10-21 | 2019-08-21 | 美國禮來大藥廠 | 組合療法 |
MX2019007104A (es) | 2016-12-15 | 2019-11-05 | Amgen Inc | Derivados de dioxido de 1,4-tiazina y dioxido de 1,2,4-tiadiazina como inhibidores de beta-secretasa y metodos de uso. |
US11548903B2 (en) | 2016-12-15 | 2023-01-10 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
JP7159161B2 (ja) | 2016-12-15 | 2022-10-24 | アムジエン・インコーポレーテツド | β-セクレターゼ阻害剤としてのシクロプロピル縮合チアジン誘導体および使用方法 |
US10947223B2 (en) | 2016-12-15 | 2021-03-16 | Amgen Inc. | Substituted oxazines as beta-secretase inhibitors |
JP7149272B2 (ja) | 2016-12-15 | 2022-10-06 | アムジエン・インコーポレーテツド | β-セクレターゼ阻害剤としてのチアジン誘導体および使用方法 |
CN116143621A (zh) * | 2022-12-14 | 2023-05-23 | 湖南农业大学 | 一种硼盐催化激活酰胺用于制备苯甲酸酯类化合物的方法 |
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GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
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US8338407B2 (en) | 2012-12-25 |
GB201101140D0 (en) | 2011-03-09 |
AR084903A1 (es) | 2013-07-10 |
CL2013002083A1 (es) | 2013-12-06 |
EP2665732A1 (en) | 2013-11-27 |
US8592408B2 (en) | 2013-11-26 |
US20130203740A1 (en) | 2013-08-08 |
AU2012208526A1 (en) | 2013-05-02 |
KR101906466B1 (ko) | 2018-10-10 |
ES2575914T3 (es) | 2016-07-04 |
ZA201303801B (en) | 2014-07-30 |
AU2012208526B2 (en) | 2015-09-24 |
IL226596A (en) | 2016-04-21 |
KR20140002724A (ko) | 2014-01-08 |
JP5947815B2 (ja) | 2016-07-06 |
PE20141182A1 (es) | 2014-09-14 |
EP2665732B1 (en) | 2016-03-30 |
NZ611365A (en) | 2015-04-24 |
JP2014502987A (ja) | 2014-02-06 |
US20140142091A1 (en) | 2014-05-22 |
TW201309710A (zh) | 2013-03-01 |
SG190908A1 (en) | 2013-07-31 |
BR112013018602A2 (pt) | 2020-09-01 |
CA2828738A1 (en) | 2012-07-26 |
RU2013138717A (ru) | 2015-02-27 |
WO2012098213A1 (en) | 2012-07-26 |
US8940734B2 (en) | 2015-01-27 |
US20120190672A1 (en) | 2012-07-26 |
CN103328486A (zh) | 2013-09-25 |
MX2013007917A (es) | 2013-08-29 |
UA109927C2 (uk) | 2015-10-26 |
CN103328486B (zh) | 2016-08-17 |
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